ackr3

CCX777 is a partial agonist recruited to ACKR3 by β-arrestin-2 and is used in cancer research.

ACKR3 agonist 1 (compound 27), exhibiting selective agonistic properties for ACKR3 (EC 50 =69 nM, E max =82%), demonstrates the capability to inhibit platelet aggregation and shows potential in mitigating platelet-mediated thrombosis. This compound is characterized by its metabolic stability and non-cytotoxic nature.

CCX-777 formic is a partial agonist that recruits β-arrestin-2 to ACKR3 (atypical chemokine receptor 3). It has applications in cancer research.

ACKR3 (CXCR7) chemokine receptor agonist

LN6023 is a ACKR3/CXCR7 Superagonist for Platelet Degranulation Modulation. LN6023 effectively reduced P-selectin expression by up to 97%, suggesting to be a potential candidate for the treatment of platelet-mediated thrombosis.

LIH383 is a peptide agonist specifically designed to activate the chemokine (C-X-C motif) receptor 7 (CXCR7), which functions both as a chemokine and an opioid peptide scavenger receptor. Demonstrating a high selectivity, LIH383 activates CXCR7 with an effective concentration (EC50) of 0.61 nM, showing significantly lower affinity towards μ-, δ-, and κ-opioid receptors, as well as the nociceptin opioid peptide (NOP) receptor, even at concentrations of 3 µM in β-arrestin recruitment assays. Furthermore, at a concentration of 3 µM, LIH383 effectively inhibits the uptake of opioid peptides by CXCR7, a process normally induced by dynorphin A, a non-selective opioid receptor agonist, in U87-ACKR3 cells.

CXCR4 antagonist and ACKR3 (CXCR7) agonist (EC50 = 350 nM for CXCR7).

trans-VUF25471 (Compound trans-3e) is a photo-switchable agonist of ACKR3. It binds to and activates ACKR3 at concentrations that are ten times lower than those required by its cis-isomer.